Assay Detail
Binding
CHEMBL617261
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In vitro affinity against serotonin 5-hydroxytryptamine 2A receptor
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.87 | 9.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL85 | RISPERIDONE | 4.0 | 1 | 9.51 |
| CHEMBL143027 | — | — | 1 | 7.97 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.56 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.28 |
| CHEMBL142668 | — | — | 1 | 6.02 |
| CHEMBL142316 | — | — | 1 | 5.90 |
| CHEMBL358895 | — | — | 1 | 5.64 |
| CHEMBL143937 | — | — | 1 | 5.08 |
| CHEMBL357517 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL85 | RISPERIDONE | Ki | = | 0.309 | nM | 9.51 |
| CHEMBL143027 | — | Ki | = | 10.72 | nM | 7.97 |
| CHEMBL42 | CLOZAPINE | Ki | = | 27.54 | nM | 7.56 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 52.48 | nM | 7.28 |
| CHEMBL142668 | — | Ki | = | 954.99 | nM | 6.02 |
| CHEMBL142316 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL358895 | — | Ki | = | 2290.87 | nM | 5.64 |
| CHEMBL143937 | — | Ki | = | 8317.64 | nM | 5.08 |
| CHEMBL357517 | — | Ki | < | 100000.0 | nM | - |